08:15 Registration & coffee

08:45 Chairman’s welcome & opening address

Prof. Mikko Niemi
MD Professor of Pharmacogenetics
Department of Clinical Pharmacology
University of Helsinki, Finland

09:00Quantification: The importance of protein quantification for the understanding of drug transporter efficacy and function in ADME

• Quantitative Targeted Absolute Proteomics (QTAP) vs. Global Proteomics (GP): Advantage and limitation
• Transporter protein quantification for ADME studies: BBB, liver and small intestine
• Transporter protein quantification for cancer research
• Advanced application of QTAP and perspective

Prof. Dr. Tetsuya Terasaki
Division of Membrane Transport and Drug targeting
Department of Biochemical Pharmacology and Therapeutics
Tohoku University, Japan

09:40In vitro screening: Transporter mediated drug-drug interactions: from in vitro screening to in vivo alteration in drugs PK

• In vitro screening of OATP1B1/3 (rOatp) and OCT1 (rOct1) inhibitors
• In vivo transporter mediated DDI
• Optimized protocol for screening large number of compounds as inhibitors of OATP1B1/3 or OCT1
• Challenges & physico-chemistry properties of OATP1B1/3 (rOatp) or OCT1 (rOct1) inhibitors

Dr. Lassina Badolo
Principal Scientist, Discovery DMPK
H. Lundbeck AS, Denmark

10:20 Refreshment break & networking

10:50In vitro techniques: Drug transporters DDI in drug development: pearls and pitfalls of in vitro experiments

• Suitable techniques for studying transporter DDI
• Assays weaknesses, bias, variability
• Designing in vitro experiment & its influence on clinical relevance
• How to apply regulations thresholds

Dr. Agnès Poirier
Group Head Drug Transport
F. Hoffmann-La Roche AG, Switzerland

11:30BBB methods: In vitro and in vivo methods to assess drug penetration at the Blood-Brain Barrier

• Challenges of drug penetration and relevant DT at the BBB
• Strategies to optimize compounds early in the drug discovery process through in vitro methods and correlation with in vivo data
• Optimization of the right parameters through optimal use of in vivo methods

Dr. Jens R. Sydor
Director DMPK
Abbott GmbH & Co. KG, Germany

12:10Discovery methods BBB: Discovery methods to obtain reliable estimates of CNS delivery – brain slice and brain to plasma unbound ratios

• Why brain to plasma unbound ratios?
• Rate and extent of transport to the brain in relation to methods available
• The brain slice method and its refinement
• Comparing brain slice and brain homogenate methods
• Combining slice and homogenate via in vivo infusion

Prof. Margareta Hammarlund-Udenaes
Department of Pharmaceutical Biosciences
Uppsala University, Sweden

12:50 Luncheon & networking

14:20 Fine tuning of brain penetration: achieving the right balance between pharmacological effects and CNS side effects

• Pharmacology and CNS effects of Gaba B PAMs
• Optimisation of in silico and in vitro parameters & POC in vivo
• Mechanistic studies in mdr1a/1b k.o. mice

Dr. Sonia-Maria Poli
Head of Non Clinical Development
Addex Pharmaceuticals, Switzerland

15:00HIV focus: Regulation of efflux drug transporters in HIV-1 neuroinflammation

• Contribution of glial cells to the neurovascular unit barrier function
• In vitro and in vivo models of HIV-1 neuroinflammation
• Functional expression of drug transporters in HIV-associated inflammation
• Complexity of antiviral drug-transporter interactions in the brain

Prof. Dr. Reina Bendayan
Pharmaceutical Sciences, Leslie Dan Faculty of Pharmacy
University of Toronto and Career Scientist Ontario HIV Treatment Network
Ministry of Health of Ontario, Canada

15:40 Refreshment break & networking

16:10 Potential implications of drug transport via intestinal and hepatic bile acid and organic anion transport proteins

• Consequences on bioavailability & toxicological potential of drug candidates according to interaction with intestinal/ hepatic DT
• In vitro and in vivo tools to examine interactions with DT
• Recent findings on the substrate specificity and transport kinetics of OATP1A2, ASBT and NTCP

Dr. Imad Hanna
Drug Metabolism and Pharmacokinetics
Novartis Institutes for BioMedical Research, USA

16:50 Drug membrane transporters assessment in hepatocyte models including HepaRG cell line

• Role of membrane transporters in drug absorption, distribution and elimination
• Relevant liver uptake and efflux transporters in DDI
• In vitro tools to study DT, including hepatocytes & comparison of different models

Dr. Firas Bassissi
DMPK Senior Scientist/Lab Head
Laboratoires Fournier/Abbott Laboratories, France

17:30 The impact of in vitro transporters on the understanding of clinical relevant DDI

• Rivaroxaban
• Kidney
• Hepatic
• Intestine

Dr. Mark Jean Gnoth
Laboratory head Bioanalytics
Bayer Pharma AG, Germany

18:10 Chairman’s closing remarks and end of the conference